[go: up one dir, main page]

MX2023007581A - C26-linked rapamycin analogs as mtor inhibitors. - Google Patents

C26-linked rapamycin analogs as mtor inhibitors.

Info

Publication number
MX2023007581A
MX2023007581A MX2023007581A MX2023007581A MX2023007581A MX 2023007581 A MX2023007581 A MX 2023007581A MX 2023007581 A MX2023007581 A MX 2023007581A MX 2023007581 A MX2023007581 A MX 2023007581A MX 2023007581 A MX2023007581 A MX 2023007581A
Authority
MX
Mexico
Prior art keywords
mtor inhibitors
rapamycin analogs
mtor
linked rapamycin
linked
Prior art date
Application number
MX2023007581A
Other languages
Spanish (es)
Inventor
Walter Won
Gert Kiss
Jennifer Pitzen
James Bradley Aggen
Arun P Thottumkara
Adrian Liam Gill
James Joseph Cregg
Gang Wang
Micah James Evans Gliedt
G Leslie Burnett
Christopher Michael Semko
Julie Chu- Li LEE
Original Assignee
Revolution Medicines Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of MX2023007581A publication Critical patent/MX2023007581A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente divulgación se relaciona con inhibidores de mTOR. Específicamente, las modalidades están dirigidas a compuestos y composiciones que inhiben mTOR, métodos de tratamiento de enfermedades mediadas por mTOR y métodos de síntesis de estos compuestos.The present disclosure relates to mTOR inhibitors. Specifically, the modalities are directed to compounds and compositions that inhibit mTOR, methods of treating mTOR-mediated diseases, and methods of synthesizing these compounds.

MX2023007581A 2018-05-01 2020-10-30 C26-linked rapamycin analogs as mtor inhibitors. MX2023007581A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862665426P 2018-05-01 2018-05-01
US201862752881P 2018-10-30 2018-10-30
US201962836040P 2019-04-18 2019-04-18

Publications (1)

Publication Number Publication Date
MX2023007581A true MX2023007581A (en) 2023-07-10

Family

ID=66625253

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020011564A MX2020011564A (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors.
MX2023007581A MX2023007581A (en) 2018-05-01 2020-10-30 C26-linked rapamycin analogs as mtor inhibitors.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2020011564A MX2020011564A (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors.

Country Status (11)

Country Link
US (2) US11685749B2 (en)
EP (1) EP3788050B1 (en)
JP (1) JP7381492B2 (en)
KR (1) KR20210018243A (en)
CN (1) CN112368289B (en)
AU (2) AU2019262979B2 (en)
CA (1) CA3098698A1 (en)
IL (2) IL312291A (en)
MX (2) MX2020011564A (en)
SG (1) SG11202010560QA (en)
WO (1) WO2019212991A1 (en)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ749959A (en) 2016-07-12 2024-12-20 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
AR110740A1 (en) 2017-01-23 2019-05-02 Revolution Medicines Inc BICYCLIC COMPOUNDS AS SHP2 ALOSTERIC INHIBITORS
JP7240320B2 (en) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド Pyridine compounds as allosteric SHP2 inhibitors
MX2020003579A (en) 2017-10-12 2020-07-22 Revolution Medicines Inc Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors.
CN111433205B (en) 2017-12-15 2024-01-19 锐新医药公司 Polycyclic compounds as allosteric SHP2 inhibitors
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
CN118978535A (en) 2018-05-01 2024-11-19 锐新医药公司 C40-, C28- and C-32-linked rapamycin analogs as mTOR inhibitors
KR20210146287A (en) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. Bicyclic heteroaryl compounds and uses thereof
JP2022522778A (en) 2019-03-01 2022-04-20 レボリューション メディシンズ インコーポレイテッド Bicyclic heterocyclyl compounds and their use
CN114867735A (en) 2019-11-04 2022-08-05 锐新医药公司 RAS inhibitors
EP4054720A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
JP2022553858A (en) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド RAS inhibitor
WO2021092115A1 (en) 2019-11-08 2021-05-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
JP2023505100A (en) 2019-11-27 2023-02-08 レボリューション メディシンズ インコーポレイテッド Covalent RAS inhibitors and uses thereof
JP2023530351A (en) 2020-06-18 2023-07-14 レヴォリューション・メディスンズ,インコーポレイテッド Methods of delaying, preventing and treating acquired resistance to RAS inhibitors
CN116209438A (en) 2020-09-03 2023-06-02 锐新医药公司 Treatment of malignant diseases with SHP2 mutations using SOS1 inhibitors
EP4214209A1 (en) 2020-09-15 2023-07-26 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
TW202241885A (en) 2020-12-22 2022-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Sos1 inhibitors and uses thereof
CN113101290A (en) * 2021-03-23 2021-07-13 徐州医科大学 Application of mTOR inhibitor Torin1 in preparation of cholestatic bile duct injury drug
TW202304863A (en) * 2021-04-09 2023-02-01 美商銳新醫藥公司 Synthesis of rapamycin analog compounds
AR125787A1 (en) 2021-05-05 2023-08-16 Revolution Medicines Inc RAS INHIBITORS
JP2024517847A (en) 2021-05-05 2024-04-23 レボリューション メディシンズ インコーポレイテッド RAS inhibitors
CN117500811A (en) 2021-05-05 2024-02-02 锐新医药公司 Covalent RAS inhibitors and uses thereof
AR127308A1 (en) 2021-10-08 2024-01-10 Revolution Medicines Inc RAS INHIBITORS
EP4448526A1 (en) 2021-12-17 2024-10-23 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CN119136806A (en) 2022-03-08 2024-12-13 锐新医药公司 Methods for treating immune-refractory lung cancer
WO2023230577A1 (en) 2022-05-25 2023-11-30 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
US20240124450A1 (en) 2022-09-21 2024-04-18 Pfizer Inc. Novel SIK Inhibitors
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
TW202446388A (en) 2023-04-14 2024-12-01 美商銳新醫藥公司 Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (156)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA737247B (en) 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
GB1459571A (en) 1974-09-12 1976-12-22 Pfizer Ltd Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus
US4316885A (en) 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4513135A (en) 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (en) 1985-10-03 1988-12-02 Merck Sharp & Dohme LIQUID-GEL PHASE TRANSITION PHARMACEUTICAL COMPOSITION
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
JPH0249775A (en) 1988-05-19 1990-02-20 Nippon Soda Co Ltd Heterocyclic compound having 6-membered or 7-membered ring and production thereof
US5120726A (en) 1991-03-08 1992-06-09 American Home Products Corporation Rapamycin hydrazones
US5023264A (en) 1990-07-16 1991-06-11 American Home Products Corporation Rapamycin oximes
JPH04230389A (en) 1990-07-16 1992-08-19 American Home Prod Corp Rapamycin derivative
US5023263A (en) 1990-08-09 1991-06-11 American Home Products Corporation 42-oxorapamycin
JPH04112877A (en) 1990-09-04 1992-04-14 Nippon Soda Co Ltd New cyanopyrazine derivative and production thereof
US5221670A (en) 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
PT98990A (en) 1990-09-19 1992-08-31 American Home Prod PROCESS FOR THE PREPARATION OF CARBOXYLIC ACID ESTERS OF RAPAMICIN
US5130307A (en) 1990-09-28 1992-07-14 American Home Products Corporation Aminoesters of rapamycin
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
EP0495421B1 (en) 1991-01-15 1996-08-21 Alcon Laboratories, Inc. Use of carrageenans in topical ophthalmic compositions
GB9103430D0 (en) 1991-02-19 1991-04-03 Smithkline Beecham Plc Novel compound
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5102876A (en) 1991-05-07 1992-04-07 American Home Products Corporation Reduction products of rapamycin
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5162333A (en) 1991-09-11 1992-11-10 American Home Products Corporation Aminodiesters of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
US5221740A (en) 1992-01-16 1993-06-22 American Home Products Corporation Oxepane isomers of rapamycin useful as immunosuppressive agents
US5177203A (en) 1992-03-05 1993-01-05 American Home Products Corporation Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
MX9304868A (en) 1992-08-13 1994-05-31 American Home Prod 27-HYDROXYRAPAMICINE, DERIVED FROM THE SAME AND PHARMACEUTICAL COMPOSITION THAT CONTAINS IT.
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5434260A (en) 1992-10-13 1995-07-18 American Home Products Corporation Carbamates of rapamycin
US5480988A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
DE69333995T2 (en) 1992-10-13 2006-10-19 Wyeth Carbamates of rapamycin
US5489680A (en) 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
US5480989A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5411967A (en) 1992-10-13 1995-05-02 American Home Products Corporation Carbamates of rapamycin
US5262423A (en) 1992-10-29 1993-11-16 American Home Products Corporation Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5260300A (en) 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
US5252579A (en) 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
AU6711994A (en) 1993-04-23 1994-11-21 American Home Products Corporation Rapamycin conjugates and antibodies
US5504091A (en) 1993-04-23 1996-04-02 American Home Products Corporation Biotin esters of rapamycin
US5387680A (en) 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5391730A (en) 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5373014A (en) 1993-10-08 1994-12-13 American Home Products Corporation Rapamycin oximes
US5378836A (en) 1993-10-08 1995-01-03 American Home Products Corporation Rapamycin oximes and hydrazones
CA2175215C (en) 1993-11-19 2008-06-03 Yat Sun Or Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5385910A (en) 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
US5385908A (en) 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
US5385909A (en) 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
BR9408323A (en) 1993-12-17 1997-08-19 Sandoz Ag Rapamycin derivatives
US5389639A (en) 1993-12-29 1995-02-14 American Home Products Company Amino alkanoic esters of rapamycin
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5463048A (en) 1994-06-14 1995-10-31 American Home Products Corporation Rapamycin amidino carbamates
US5491231A (en) 1994-11-28 1996-02-13 American Home Products Corporation Hindered N-oxide esters of rapamycin
US5563145A (en) 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US5741677A (en) 1995-06-07 1998-04-21 Geron Corporation Methods for measuring telomere length
AU712193B2 (en) 1995-06-09 1999-10-28 Novartis Ag Rapamycin derivatives
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
CN1226245A (en) 1996-06-20 1999-08-18 德克萨斯州大学系统董事会 Pharmacologically active compound, its preparation method and use
US6342507B1 (en) 1997-09-05 2002-01-29 Isotechnika, Inc. Deuterated rapamycin compounds, method and uses thereof
JP2002508971A (en) 1998-01-15 2002-03-26 アリアド・ジーン・セラピューティクス・インコーポレーテッド Regulation of biological events using multimeric chimeric proteins
CN1293081C (en) 1999-08-24 2007-01-03 阿里亚德基因治疗公司 28-epirapalogs
US6277983B1 (en) 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
EP3406249A1 (en) 2001-02-19 2018-11-28 Novartis AG Treatment of breast tumors with a rapamycin derivative in combination with an aromatase inhibitor
US20040116444A1 (en) 2002-09-12 2004-06-17 Corbett Jeffrey W. Substituted 1,4-pyrazine derivatives
JP2004161716A (en) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Jnk inhibitor
US7160867B2 (en) 2003-05-16 2007-01-09 Isotechnika, Inc. Rapamycin carbohydrate derivatives
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
CA2528173A1 (en) 2003-07-16 2005-02-03 Wyeth Cci-779 isomer c
US7220755B2 (en) 2003-11-12 2007-05-22 Biosensors International Group, Ltd. 42-O-alkoxyalkyl rapamycin derivatives and compositions comprising same
DE602005011879D1 (en) 2004-03-01 2009-02-05 Terumo Corp Process for the preparation of O-alkylated rapamycin derivatives
KR20070008709A (en) 2004-04-30 2007-01-17 다케다 야쿠힌 고교 가부시키가이샤 Heterocyclic Amide Compounds and Their Uses as MMP-13 Inhibitors
CN100516195C (en) 2004-07-19 2009-07-22 汕头市双骏生物科技有限公司 New strain and method of producing pacilitaxel using said strain
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
EP1838288A4 (en) 2004-12-20 2010-08-04 Ariad Pharma Inc Therapeutic materials and methods
AU2006221024A1 (en) 2005-03-07 2006-09-14 Wyeth Oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin
US7189582B2 (en) * 2005-04-27 2007-03-13 Dade Behring Inc. Compositions and methods for detection of sirolimus
TW200700403A (en) 2005-05-20 2007-01-01 Solvay Process for preparing an epoxide from a polyhydroxylated aliphatic hydrocarbon and a chlorinating agent
EP1942807A1 (en) 2005-10-27 2008-07-16 Koninklijke Philips Electronics N.V. Using tissue acceleration to create better dit waveforms (doppler tissue imaging) for crt (cardiac resynchronization therapy)
CN102936250B (en) 2005-11-17 2014-07-09 Osi医药有限责任公司 Fused bicyclic mtor inhibitors
US9006224B2 (en) 2005-11-21 2015-04-14 Novartis Ag Neuroendocrine tumor treatment
GB0525546D0 (en) 2005-12-15 2006-01-25 Novartis Ag Organic compounds
DK2004654T3 (en) 2006-04-04 2013-07-22 Univ California Pyrazolopyrimidine derivatives for use as kinase antagonists
US20090274739A1 (en) 2006-04-13 2009-11-05 The Trustees Of Columbia University In The City Of New York Methods and compositions for treating neointimal hyperplasia
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
FR2903038B1 (en) 2006-06-29 2009-04-17 Facom Sa SUPPORT FOR A SERIES OF TOOLS.
MY148688A (en) 2006-08-23 2013-05-31 Kudos Pharm Ltd 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
JP5306818B2 (en) 2006-10-18 2013-10-02 武田薬品工業株式会社 Fused heterocyclic compounds
EP1916006A1 (en) 2006-10-19 2008-04-30 Albert Schömig Implant coated with a wax or a resin
EP2090580B1 (en) 2006-11-27 2014-06-04 Terumo Kabushiki Kaisha Process for producing o-alkylated rapamycin derivative, and o-alkylated rapamycin derivative
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
CA2678415A1 (en) 2007-04-05 2008-10-16 Wyeth Wortmannin-rapamycin conjugate and uses thereof
JPWO2008156174A1 (en) 2007-06-21 2010-08-26 大正製薬株式会社 Pyrazineamide compound
US20090074831A1 (en) 2007-09-18 2009-03-19 Robert Falotico LOCAL VASCULAR DELIVERY OF mTOR INHIBITORS IN COMBINATION WITH PEROXISOME PROLIFERATORS-ACTIVATED RECEPTOR STIMULATORS
WO2009046436A1 (en) 2007-10-04 2009-04-09 Memorial Sloan-Kettering Cancer Center Methods for inhibiting senescence of epithelial cells
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
KR101897881B1 (en) 2008-01-04 2018-09-12 인텔리카인, 엘엘씨 Certain chemical entities, compositions and methods
US7842475B2 (en) * 2008-01-08 2010-11-30 Siemens Healthcare Diagnostics Inc. Stabilization of solid support assay reagents
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
US20090253733A1 (en) 2008-04-02 2009-10-08 Biointeractions, Ltd. Rapamycin carbonate esters
WO2009131631A1 (en) 2008-04-14 2009-10-29 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
TW200948361A (en) 2008-05-26 2009-12-01 Chunghwa Chemical Synthesis & Biotech Co Ltd Method for synthesizing Biolimus A9 and the like and method for improving stability of the same
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
AU2009268611B2 (en) 2008-07-08 2015-04-09 Intellikine, Llc Kinase inhibitors and methods of use
US20100055145A1 (en) 2008-08-29 2010-03-04 Biosensors International Group Stent coatings for reducing late stent thrombosis
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
DK2358720T3 (en) 2008-10-16 2016-06-06 Univ California Heteroarylkinaseinhibitorer fused-ring
CN102256966B (en) 2008-10-17 2016-02-10 白头生物医学研究所 Soluble mTOR complex and its regulators
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
US20110269779A1 (en) 2008-11-18 2011-11-03 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
US8637499B2 (en) 2009-05-26 2014-01-28 Exelixis, Inc. Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture
SG10201404886PA (en) 2009-08-17 2014-10-30 Intellikine Llc Heterocyclic compounds and uses thereof
BR112012003637A2 (en) 2009-08-17 2017-04-25 Memorial Sloan Kettering Cancer Center "heat shock protein binding compounds, compositions, and methods for preparing and using them"
WO2011047384A2 (en) 2009-10-16 2011-04-21 The Regents Of The University Of California Methods of inhibiting ire1
ES2593256T3 (en) 2010-05-21 2016-12-07 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulations
WO2012017449A1 (en) 2010-08-04 2012-02-09 Meril Life Sciences Pvt. Ltd Process for preparation of novel 42-0-(heteroalkoxyalkyl) rapamycin compounds with anti-proliferative properties"
JP5847386B2 (en) 2010-09-15 2016-01-20 関東化學株式会社 Method for producing amine compound
WO2012066502A1 (en) 2010-11-19 2012-05-24 Biocon Limited Processes for preparation of everolimus and intermediates thereof
EP4230631A3 (en) 2011-02-04 2024-03-27 Synthon B.V. Process for making trisubstituted silyloxyethyl triflates
WO2012148540A1 (en) 2011-02-23 2012-11-01 Intellikine, Llc Combination of kanase inhibitors and uses threof
US20140357651A1 (en) 2011-05-04 2014-12-04 Yi Liu Combination pharmaceutical compositions and uses thereof
JP6122420B2 (en) 2011-05-06 2017-04-26 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Treatment of multiple cystic diseases
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
KR20150003156A (en) 2012-11-30 2015-01-08 항조우 질록스 파마 컴퍼니 리니티드 Rapamycin analogs and methods for making the same
WO2015066371A1 (en) 2013-10-31 2015-05-07 Forum Pharmaceuticals, Inc. SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
JP6701077B2 (en) 2013-12-19 2020-05-27 シアトル ジェネティックス, インコーポレイテッド Methylene carbamate linker for use with targeted drug conjugates
CN105461738B (en) 2014-06-03 2019-03-08 中国人民解放军军事医学科学院毒物药物研究所 A kind of rapamycin derivative, preparation method, its pharmaceutical composition and purposes
KR101668590B1 (en) 2014-06-19 2016-10-25 전남대학교병원 Bioactive Peptide-coated Stent Promotes Endothelial Cell Proliferation and Prevents Stent Thrombosis
WO2016040806A1 (en) * 2014-09-11 2016-03-17 The Regents Of The University Of California mTORC1 INHIBITORS
WO2016100116A1 (en) * 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
US20160279108A1 (en) 2015-02-24 2016-09-29 University Of Kansas Targeted mtor inhibitors
CN106188093B (en) 2015-05-08 2018-06-12 上海医药工业研究院 A kind of rapamycin structure analog and preparation method thereof
WO2017044720A1 (en) * 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
SI3402792T1 (en) 2016-01-11 2022-01-31 Merck Patent Gmbh Quinolin-2-one derivatives
WO2018014858A1 (en) 2016-07-21 2018-01-25 正大天晴药业集团股份有限公司 M-dihydroxybenzene derivative crystal and salt, and manufacturing method thereof
KR20200012876A (en) * 2017-05-02 2020-02-05 레볼루션 메디슨즈, 인크. Paramycin Analogues as mTOR Inhibitors
AR112834A1 (en) 2017-09-26 2019-12-18 Novartis Ag RAPAMYCIN DERIVATIVES
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
CN118978535A (en) 2018-05-01 2024-11-19 锐新医药公司 C40-, C28- and C-32-linked rapamycin analogs as mTOR inhibitors
WO2020160711A1 (en) 2019-02-07 2020-08-13 Beigene, Ltd. Imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivatives as tlr7 agonist
JP2023530351A (en) 2020-06-18 2023-07-14 レヴォリューション・メディスンズ,インコーポレイテッド Methods of delaying, preventing and treating acquired resistance to RAS inhibitors
TW202304863A (en) 2021-04-09 2023-02-01 美商銳新醫藥公司 Synthesis of rapamycin analog compounds
WO2023230577A1 (en) 2022-05-25 2023-11-30 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor

Also Published As

Publication number Publication date
CN112368289A (en) 2021-02-12
MX2020011564A (en) 2021-01-29
IL278335B2 (en) 2024-09-01
US20220340596A1 (en) 2022-10-27
IL278335B1 (en) 2024-05-01
IL278335A (en) 2020-12-31
US11685749B2 (en) 2023-06-27
US20240166667A1 (en) 2024-05-23
KR20210018243A (en) 2021-02-17
EP3788050A1 (en) 2021-03-10
JP2021523113A (en) 2021-09-02
AU2019262979A1 (en) 2020-12-10
AU2019262979B2 (en) 2023-07-06
CA3098698A1 (en) 2019-11-07
CN112368289B (en) 2024-02-20
SG11202010560QA (en) 2020-11-27
WO2019212991A1 (en) 2019-11-07
US12187746B2 (en) 2025-01-07
EP3788050B1 (en) 2024-08-28
JP7381492B2 (en) 2023-11-15
IL312291A (en) 2024-06-01
AU2023241273A1 (en) 2023-10-26

Similar Documents

Publication Publication Date Title
MX2023007581A (en) C26-linked rapamycin analogs as mtor inhibitors.
MX2020011565A (en) C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors.
MX2023000410A (en) Rapamycin analogs as mtor inhibitors.
DOP2022000082A (en) BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
CO2017011484A2 (en) Bromodomain inhibitors
PH12018500177A1 (en) Compositions useful for treating disorders related to kit and pdfgr
CO2018004964A2 (en) Useful compounds as immunomodulators
ECSP17073191A (en) HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS
EA201892147A1 (en) BICYCLIC COMPOUNDS
MX380092B (en) TREATMENT OF OSTEOARTHRITIS.
EA201890308A1 (en) SUBSTITUTED ASO COMPOUNDS AS IRAK-4 INHIBITORS
EA201591382A1 (en) INHIBITORS OF GISTONDEMETILAZ
BR112018003026A2 (en) compositions comprising a pi3k inhibitor and an hdac inhibitor
CU24410B1 (en) BENZIMIDAZOL-2-AMINAS AS MIDH1 INHIBITORS
EA201792021A1 (en) JAK INHIBITOR
TR201906366T4 (en) Synthesis of polycyclic-carbamoylpyridone compounds.
MX2018014330A (en) Aminoacylindazole immunomodulators for treatment of autoimmune diseases.
UY37017A (en) AZA-BENCIMIDAZOL INHIBITORS OF PAD4
EA201792425A1 (en) TRICYCLIC COMPOUNDS AND THEIR APPLICATION AS PHOSPHODYSTERASE INHIBITORS
MX373603B (en) KCNQ2-5 CHANNEL ACTIVATOR.
EA202090900A1 (en) IMMUNOPROTEASOM INHIBITORS
EA201990362A1 (en) ANALOGUE OF VORTIOXETINE AND ITS APPLICATION AND OBTAINING
MX2019002017A (en) Sofosbuvir derivatives for the treatment of hepatitis c.
EA201690400A1 (en) SUBSTITUTED IMIDAZOLES USED AS BLOCATORS OF N-TYPE CALCIUM CHANNELS
EA201892698A1 (en) DERIVATIVES OF PYRAZOLYLAMINOBENZIMIDAZOLE AS A JAK INHIBITORS